Ecdysterone is a joint name of a kind of natural products that were first discovered in insects. Ecdysterones have molting activity, as well as the effect for promoting cell growth. After 1960s, people found that ecdysterones are also present in plants. Their distribution in plants is higher and wider than that in animals. The ecdysterones are widely present in plants such as Twotoothed Achyranthes Root, Mulberry Leaf, rhaponticum uniflorum and the like. The amounts of ecdysterones in insect body are extremely low. Therefore, currently plant ecdysterones are the main source of commercial ecdysterones. The researches show that ecdysterones possess a variety of pharmacological actions, such as promoting the synthesis of ribonucleic acid and protein, effecting the saccharometabolism, promoting lipid metabolism, immunoloregulation, effecting central nervous system, anti-oxidation, activating blood circulation to dissipate blood stasis and the like.
Chinese Patent CN 1280010A published at Jan. 17, 2001 to Chongren Yang et al. discloses an oral medicament for treating diabetes comprising β-ecdysone and 2-β-ecdysone acetate as the medicinal active ingredients in a weight ratio of 50-95% β-ecdysone to 5-50% 2-β-ecdysone acetate.
Chinese Patent CN 1557324A published at Dec. 29, 2004 to Qiu Chen et al. discloses the use of ecdysterone in preparation of a medicament for treating insulin resistance.
“The effect of ecdysterone on glucose consumption of HepG2 cells” in CHINESE PHARMACOLOGICAL BULLETIN, vol 11, 2005, Qiu Chen et al. discloses that the ecdysterone in a concentration range of 1×10−6˜10−4 mol·L−1 increases the glucose consumption of HepG2 cells (by 44%˜77%); the effect of ecdysterone on lowering glucose decreases as the increase of glucose concentration in culture solution; and insulin does not obviously effect the action of ecdysterone for lowering glucose. Ecdysterone does not have the action of stimulating insulin secretion of β-TC3 cells, which suggests that ecdysterone can play a non-insulin dependent function of lowering glucose through hepatocyte, but cannot stimulate insulin secretion.
“The effect of ecdysterone on protein expression of insulin receptor in insulin resistant HepG2 cells”, SHANDONG MEDICAL JOURNAL, vol 04, 2008, Qiu Chen et al. discloses that 1×10−5 mol/L of ecdysterone significantly increases the expression of InsR protein in IR HepG2 cells, showing that insulin sensitization by ecdysterone may be associated with the increased expression of InsR protein, an insulin signal transduction molecule.
“The effect of ecdysterone on the protein expression of PI3K, Glut-4 in insulin resistant HepG2 cells”, JIANGSU MEDICAL JOURNAL, vol 3, 2009 Chen et al. discloses that 1×10−5M ecdysterone increases the expression of PI3K and GLUT-4 proteins in insulin resistant HepG2 cells (P<0.05), showing that insulin sensitization by ecdysterone may be associated with the increased expression of PI3K and GLUT-4 proteins which are insulin signal transduction molecules.
“A proteomic study on the insulin resistant HepG2 cell treated by ecdysterone”, CHINESE PHARMACOLOGICAL BULLETIN, vol 12, 2009, Min Song et al. discloses the effect of ecdysterone on glucose consumption in insulin resistant model cells, showing that the targets for insulin sensitization by ecdysterone relate to a variety of insulin resistance related proteins and kinases.
In addition, ecdybase.org discloses separated phosphate derivatives of ecdysterone as follows:
1. 26-hydroxyecdysterone-2-phosphate (THOMPSON, J. A. et al., (1987) Arch. Insect Biochem. Physiol. 4, 183-190);
2. 26-hydroxyecdysterone-26-phosphate (THOMPSON, M. J. et al., (1985) Arch. Insect Biochem. Physiol. 2, 227-236);
3. 20-hydroxyecdysterone-22-phosphate (TSOUPRAS, G. et al., (1982) Steroids 40, 551-560);
4. 20-hydroxyecdysterone-3-acetate2-phosphate (ISAAC, R. E. et al., (1984) Biochem. J. 231, 459-464);
5. 20-hydroxyecdysterone-3(2)-phosphate (TSOUPRAS, G. et al., (1983) C. R. Acad. Sci. Paris, Sér. III, 296, 77-80);
6. 20-hydroxyecdysterone-3(2)-acetate-22-phosphate (TSOUPRAS, G. et al., (1983) C. R. Acad. Sci. Paris, Sér. III, 296, 77-80);
7. ecdysterone-3-phosphate (TSOUPRAS, G. et al., (1982) (Thesis, Strasbourg, France));
8. ecdysterone-2-phosphate (ISAAC, R. E. et al., (1984) Biochem. J. 217, 239-243);
9. ecdysterone-2,3-diacetate-22-phosphate (TSOUPRAS, G. et al., (1982) (Thesis, Strasbourg, France));
10. ecdysterone-2-acetate-3-phosphate (ISAAC, R. E. et al., (1984) Biochem. J. 217, 239-243);
11. ecdysterone-3(2)-acetate-22-phosphate (ISAAC, R. E. et al., (1984) Biochem. J. 231, 459-464).